Cediranib Maleate

For research use only.

Catalog No.S5242 Synonyms: AZD-2171 maleate

3 publications

Cediranib Maleate Chemical Structure

CAS No. 857036-77-2

Cediranib Maleate (AZD-2171) is the maleate salt of Cediranib, which is a potent inhibitor of VEGFR with IC50 of <1 nM and also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.

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Biological Activity

Description Cediranib Maleate (AZD-2171) is the maleate salt of Cediranib, which is a potent inhibitor of VEGFR with IC50 of <1 nM and also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.
Targets
VEGFR2/KDR [2]
(HUVECs)
c-Kit [2]
(HUVECs)
c-Kit [2]
(HUVECs)
VEGFR3/FLT4 [2]
(HUVECs)
VEGFR1/FLT1 [2]
(HUVECs)
0.5 nM 2 nM 2 nM <=3 nM 5 nM
In vitro

In recombinant kinase assays, cediranib inhibits VEGFR-1 kinase activity (IC50 = 5 nmol/L) within a similar concentration range to VEGFR-2 and VEGFR-3 (IC50 values of <0.1 and ≤3 nmol/L). It shows selectivity against other kinases. Cediranib has similar potency against c-Kit when compared with VEGFR-2 in phosphorylation assays but less potency against PDGFR-α and PDGFR-β, particularly in a PDGF-AA/PDGFR-α–driven tumor cell proliferation assay. Cediranib is inactive against wild-type Flt-3 (IC50 value >1 μmol/L) and had marginal activity versus FGFR-1 and -4 (IC50 values of 0.35 and 2.17 μmol/L, respectively)[1].

In vivo Phosphorylation of wild-type c-Kit in NCI-H526 tumor xenografts was reduced markedly following oral administration of cediranib (≥1.5 mg/kg/d) to tumor-bearing nude mice[1].

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (176.49 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 566.58
Formula

C25H27FN4O3.C4H4O4

CAS No. 857036-77-2
Storage powder
in solvent
Synonyms AZD-2171 maleate
Smiles CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCC5.C(=CC(=O)O)C(=O)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01116648 Active not recruiting Drug: Cediranib|Drug: Cediranib Maleate|Drug: Olaparib Ovarian Endometrioid Adenocarcinoma|Ovarian Serous Adenocarcinoma|Ovarian Serous Surface Papillary Adenocarcinoma|Recurrent Breast Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Triple-Negative Breast Carcinoma National Cancer Institute (NCI) March 25 2010 Phase 1|Phase 2
NCT00458731 Completed Biological: bevacizumab|Drug: cediranib maleate Adult Grade III Lymphomatoid Granulomatosis|Adult Nasal Type Extranodal NK/T-cell Lymphoma|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Childhood Burkitt Lymphoma|Childhood Diffuse Large Cell Lymphoma|Childhood Grade III Lymphomatoid Granulomatosis|Childhood Immunoblastic Large Cell Lymphoma|Childhood Nasal Type Extranodal NK/T-cell Lymphoma|Cutaneous B-cell Non-Hodgkin Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Hepatosplenic T-cell Lymphoma|Intraocular Lymphoma|Nodal Marginal Zone B-cell Lymphoma|Noncutaneous Extranodal Lymphoma|Peripheral T-cell Lymphoma|Progressive Hairy Cell Leukemia Initial Treatment|Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult Immunoblastic Large Cell Lymphoma|Recurrent Adult Lymphoblastic Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Childhood Anaplastic Large Cell Lymphoma|Recurrent Childhood Large Cell Lymphoma|Recurrent Childhood Lymphoblastic Lymphoma|Recurrent Childhood Small Noncleaved Cell Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Recurrent/Refractory Childhood Hodgkin Lymphoma|Refractory Hairy Cell Leukemia|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|Stage IV Adult Burkitt Lymphoma|Stage IV Adult Diffuse Large Cell Lymphoma|Stage IV Adult Diffuse Mixed Cell Lymphoma|Stage IV Adult Diffuse Small Cleaved Cell Lymphoma|Stage IV Adult Hodgkin Lymphoma|Stage IV Adult Immunoblastic Large Cell Lymphoma|Stage IV Adult Lymphoblastic Lymphoma|Stage IV Adult T-cell Leukemia/Lymphoma|Stage IV Childhood Anaplastic Large Cell Lymphoma|Stage IV Childhood Hodgkin Lymphoma|Stage IV Childhood Large Cell Lymphoma|Stage IV Childhood Lymphoblastic Lymphoma|Stage IV Childhood Small Noncleaved Cell Lymphoma|Stage IV Grade 1 Follicular Lymphoma|Stage IV Grade 2 Follicular Lymphoma|Stage IV Grade 3 Follicular Lymphoma|Stage IV Mantle Cell Lymphoma|Stage IVA Mycosis Fungoides/Sezary Syndrome|Stage IVB Mycosis Fungoides/Sezary Syndrome|T-cell Large Granular Lymphocyte Leukemia|Testicular Lymphoma|Unspecified Adult Solid Tumor Protocol Specific|Unspecified Childhood Solid Tumor Protocol Specific|Waldenström Macroglobulinemia National Cancer Institute (NCI) May 2007 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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VEGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID